concept

5-HT2AR

Facts (10)

Sources

Neuroimaging in psychedelic drug development: past, present, and ... nature.com Nature Sep 27, 2023 8 facts

claimEstimating the relationship between plasma concentration and 5-HT2AR occupancy following repeat-dose administration is considered obligatory data for determining dosing in Phase II and Phase III studies in modern CNS drug development.

claimResearchers reported that neocortical 5-HT2AR binding is negatively associated with the peak plateau duration of the psilocybin experience.

claimThe 5-HT2AR agonist PET ligand [11C]Cimbi-36 has higher sensitivity to serotonin receptor agonists and has been used to demonstrate that the acute subjective effects of psilocybin (specifically its active metabolite psilocin) are related to its binding at 5-HT2A receptors.

claimA study examined the relationship between 5-HT2AR binding measured with PET and long-term changes in personality factors.

claimThe use of Positron Emission Tomography (PET) for molecular imaging of psychedelics has been limited by high costs, ethical and methodological difficulties, and a lack of suitable 5-HT2AR agonist PET radioligands.

procedure[11C]CIMBI-36 PET can be used to establish the relationship between drug plasma concentration and 5-HT2AR occupancy.

referenceA precision psychiatry approach proposed by researchers (cited as [97]) suggests that variability in individual acute and long-term clinical responses to psychedelics could be captured by computational approaches leveraging resting-state fMRI data combined with population-level maps of the 5-HT2AR and gene expression data.

claimInteractions between conventional psychiatric treatments like SSRIs and psychedelic drugs can occur at multiple levels, including peripheral pharmacokinetic interactions, central pharmacokinetic interactions (such as competition at the 5-HT2AR), or pharmacodynamic interactions affecting second messenger systems or neuroplasticity.

Effects of psychedelics on neurogenesis and broader neuroplasticity link.springer.com Springer Dec 19, 2024 2 facts

claimThe effects of psychedelics on neurogenesis and neuroplasticity appear to be modulated by serotonin receptors, specifically 5-HT2BR and 5-HT2AR.

claimIn ex vivo slices from P14-P21 mice, 1µM DOI induced Long-Term Depression (LTD) in mPFC layer 5 pyramidal neurons, reducing the amplitude of AMPA excitatory postsynaptic currents (EPSC) from layer 1 pyramidal stimuli by nearly half; this effect was mediated by 5-HT2AR and required the internalization of GluA2-containing AMPA receptors via Protein kinase C (PKC).